公开(公告)号：US09834526B2

公开(公告)日：2017-12-05

申请号：US15104510

申请日：2014-12-17

Applicant: MERCK SHARP & DOHME CORP. ,  MERCK CANADA INC.

Inventor： John A. McCauley ,  Christian Beaulieu ,  David Jonathan Bennett ,  Christopher J. Bungard ,  Sheldon Crane ,  Thomas J. Greshock ,  Katharine M. Holloway ,  Daniel McKay ,  Carmela Molinaro ,  Oscar Miguel Moradei ,  Satyanarayana Tummanapalli ,  Vouy Linh Truong ,  Peter D. Williams

IPC: A61K31/535 ,  C07D265/28 ,  C07D265/30 ,  A61K45/06 ,  A61K31/5375 ,  A61K31/5377 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

CPC classification number: C07D265/30 ,  A61K31/5375 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: The present invention is directed to 2,5,6-substituted morpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

公开(公告)号：US11655216B2

公开(公告)日：2023-05-23

申请号：US16341595

申请日：2017-10-09

Applicant: Merck Sharp & Dohme Corp. ,  Michael T. Rudd ,  Zhaoyang Meng ,  Jenny Wai ,  David Jonathan Bennett ,  Edward J. Brnardic ,  Nigel J. Liverton ,  Shawn J. Stachel ,  Yongxin Han ,  Paul Tempest ,  Jiuxiang Zhu ,  Xuewang Xu ,  Bin Zhu

Inventor： Michael T. Rudd ,  Zhaoyang Meng ,  Jenny Wai ,  David Jonathan Bennett ,  Edward J. Brnardic ,  Nigel J. Liverton ,  Shawn J. Stachel ,  Yongxin Han ,  Paul Tempest ,  Jiuxiang Zhu ,  Xuewang Xu ,  Bin Zhu

IPC: C07D221/20 ,  C07D401/12 ,  C07D417/12 ,  C07D405/12 ,  C07D211/22 ,  C07D401/14 ,  C07D417/14

CPC classification number: C07D221/20 ,  C07D211/22 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14

Abstract: In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US20210403469A1

公开(公告)日：2021-12-30

申请号：US17289062

申请日：2019-11-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Yongxin Han ,  David Jonathan Bennett ,  Indu Bharathan ,  Liangqin Guo ,  Brett A. Hopkins ,  Xianhai Huang ,  Derun Li ,  Min Lu ,  Alexander Pasternak ,  David L. Sloman ,  Hongjun Zhang ,  Hua Zhou

IPC: C07D471/04 ,  C07D401/04 ,  C07D215/14 ,  C07D209/94 ,  C07D403/04

Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Formula (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US10894775B2

公开(公告)日：2021-01-19

申请号：US16341591

申请日：2017-10-09

Applicant: Merck Sharp & Dohme Corp. ,  Michael T. Rudd ,  Zhaoyang Meng ,  Jenny Wai ,  David Jonathan Bennett ,  Edward J. Brnardic ,  Nigel J. Liverton ,  Shawn J. Stachel ,  Yongxin Han ,  Paul Tempest ,  Jiuxiang Zhu ,  Xuewang Xu ,  Bin Zhu ,  Chuanman Huang

Inventor： Michael T. Rudd ,  Zhaoyang Meng ,  Jenny Wai ,  David Jonathan Bennett ,  Edward J. Brnardic ,  Nigel J. Liverton ,  Shawn J. Stachel ,  Yongxin Han ,  Paul Tempest ,  Jiuxiang Zhu ,  Xuewang Xu ,  Bin Zhu ,  Chuanman Huang

IPC: C07D221/20 ,  C07D211/16 ,  C07D211/96

Abstract: In its many embodiments, the present invention provides certain piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US20180354901A1

公开(公告)日：2018-12-13

申请号：US15780289

申请日：2016-11-29

Applicant: Michael T. Rudd ,  David Jonathan Bennett ,  Jenny Wai ,  Zhaoyang Meng ,  Merck Sharp & Dohme Corp.

Inventor： Michael T. Rudd ,  David Jonathan Bennett ,  Jenny Wai ,  Zhaoyang Meng

IPC: C07D211/16 ,  C07D401/14 ,  C07D211/44 ,  C07D409/14 ,  C07D401/06 ,  C07D487/08 ,  C07D413/14 ,  C07D417/14 ,  C07D451/02

Abstract: In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein ring A, ring B, R1, R2, R3, L, R4, X, Z, Li, Q and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US20180305332A1

公开(公告)日：2018-10-25

申请号：US15774655

申请日：2016-11-07

Applicant: Merck Sharp & Dohme Corp.

Inventor： Shawn J. Stachel ,  David Jonathan Bennett ,  Edward J. Brnardic ,  Nigel J. Liverton ,  Peter J. Manley ,  Zhaoyang Meng ,  Kausik K. Nanda ,  Michael T. Rudd ,  Jenny Wai

IPC: C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D471/10 ,  C07D417/14 ,  C07D405/14

CPC classification number: C07D401/04 ,  A61K31/451 ,  C07D211/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/10

Abstract: In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, Q and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US09737545B2

公开(公告)日：2017-08-22

申请号：US15104782

申请日：2014-12-17

Applicant: MERCK SHARP & DOHME CORP. ,  MERCK CANADA INC.

Inventor： John A. McCauley ,  Christian Beaulieu ,  David Jonathan Bennett ,  Christopher J. Bungard ,  Sheldon Crane ,  Thomas J. Greshock ,  Katharine M. Holloway ,  Helen Juteau ,  Daniel McKay ,  Carmela Molinaro ,  Oscar Miguel Moradei ,  Christian Nadeau ,  Daniel Simard ,  Satyanarayana Tummanapalli ,  Vouy Linh Truong ,  Karine M. Villeneuve ,  Peter D. Williams

IPC: A61K31/5377 ,  C07D417/04 ,  A61K45/06 ,  C07D487/04 ,  C07D471/04 ,  C07D413/04 ,  C07D265/30 ,  C07D413/14

CPC classification number: A61K31/5377 ,  A61K45/06 ,  C07D265/30 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention is directed to 5-heteroarylmorpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

公开(公告)号：US20160311786A1

公开(公告)日：2016-10-27

申请号：US15104510

申请日：2014-12-17

Applicant: MERCK SHARP & DOHME CORP. ,  MERCK CANADA INC.

Inventor： John A. McCauley ,  Christian Beaulieu ,  David Jonathan Bennett ,  Christopher J. Bungard ,  Sheldon Crane ,  Thomas J. Greshock ,  Katharine M. Holloway ,  Daniel McKay ,  Carmela Molinaro ,  Oscar Miguel Moradei ,  Satyanarayana Tummanapalli ,  Vouy Linh Truong ,  Peter D. Williams

IPC: C07D265/30 ,  A61K45/06 ,  C07D413/12 ,  A61K31/5377 ,  C07D471/04 ,  C07D417/14 ,  C07D487/04 ,  C07D417/12 ,  C07D513/04 ,  A61K31/5375 ,  C07D413/14

CPC classification number: C07D265/30 ,  A61K31/5375 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: The present invention is directed to 2,5,6-substituted morpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract translation: 本发明涉及2,5,6-取代的吗啉衍生物及其在抑制HIV蛋白酶，HIV复制抑制，HIV感染预防，HIV感染治疗和预防治疗中的应用 ，并延迟艾滋病的发病或进展。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

公开(公告)号：US20150166520A1

公开(公告)日：2015-06-18

申请号：US14415885

申请日：2013-07-16

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Paul J. Coleman ,  Abbas M. Walji ,  Qun Dang ,  David Jonathan Bennett ,  Sophie D. Clas ,  John S. Wai ,  Jaume Balsells-Padros ,  Henry Y. Wu ,  Ronald L. Smith ,  Rebecca Nofsinger ,  Rosa I. Sanchez

IPC: C07D413/12 ,  A61K45/06 ,  A61K31/513

CPC classification number: C07D413/12 ,  A61K31/427 ,  A61K31/513 ,  A61K31/52 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention relates to Amido-Substituted Pyrimidinone Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Pyrimidinone Derivative, and methods of using the Amido-Substituted Pyrimidinone Derivatives for treating or preventing HIV infection in a subject.

Abstract translation: 本发明涉及式（I）的酰胺取代的嘧啶酮衍生物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5和R 6如本文所定义。 本发明还涉及包含至少一种酰胺取代的嘧啶酮衍生物的组合物，以及使用酰胺取代的嘧啶酮衍生物来治疗或预防受试者中HIV感染的方法。